- Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2Creceptor
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The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT2Creceptor agonists are reported. An early lead containing a highly unique 6,6,7-ring system was optimized for both in vitro potency and selectivity at the related 5-HT2Breceptor. Orally bioactive, potent, and selective 6,6,6-tricyclic 5-HT2Cagonists were identified.
- Schrader, Thomas O.,Kasem, Michelle,Ren, Albert,Feichtinger, Konrad,Al Doori, Bilal,Wei, Jing,Wu, Chunrui,Dang, Huong,Le, Minh,Gatlin, Joel,Chase, Kelli,Dong, Jenny,Whelan, Kevin T.,Sage, Carleton,Grottick, Andrew J.,Semple, Graeme
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supporting information
p. 5877 - 5882
(2016/12/06)
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- Triflic anhydride mediated synthesis of imidazo[1,5-a]azines
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Imidazo[1,5-a]azines are synthesized in moderate to excellent yields using a mild cyclodehydration/aromatization reaction triggered by the use of triflic anhydride (Tf2O) and 2-methoxypyridine (2-MeOPyr). Various substitution patterns and functional groups were found to be compatible under the optimized conditions. In addition, a 5-bromo-3-aryl derivative was also shown to be active in a Sonogashira cross-coupling and direct arylation reactions. A tertiary amide was compatible as a substrate leading to the synthesis of an imidazo[1,5-a]pyridinium triflate.
- Pelletier, Guillaume,Charette, Andre B.
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p. 2290 - 2293
(2013/06/26)
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- Synthesis of amidomethyltrifluoroborates and their use in cross-coupling reactions
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Amidomethyltrifluoroborates were successfully synthesized in a one-pot fashion and used in cross-coupling reactions with a wide variety of aryl and heteroaryl chlorides.
- Molander, Gary A.,Hiebel, Marie-Aude
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supporting information; experimental part
p. 4876 - 4879
(2010/12/25)
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